ALK-IN-1 (Brigatinib analog, AP26113 analog)

Catalog No.: A11948
ALK inhibitor
AP26113 is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line. In a panel of EML4-ALK or NPM-ALK-positive cell lines, AP26113 has IC50 values of 4-31 nM. [1][2] AP26113 is effective against sensitive and resistant H3122 cells, reducing cell growth, suppressing ALK phosphorylation, and inducing apoptosis. In Ba/F3 cells expressing native or mutant EML4-ALK, AP26113 was active at IC50s of 10 and 24 nM, respectively. [3]
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Product Name Price Stock Qty
AP26113 5mg
$55.00
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AP26113 10mg
$75.00
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AP26113 25mg
$110.00
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AP26113 50mg
$160.00
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AP26113 10mM * 1mL in DMSO
$120.00
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Biological Activity
Discription AP26113 is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line. In a panel of EML4-ALK or NPM-ALK-positive cell lines, AP26113 has IC50 values of 4-31 nM. [1][2] AP26113 is effective against sensitive and resistant H3122 cells, reducing cell growth, suppressing ALK phosphorylation, and inducing apoptosis. In Ba/F3 cells expressing native or mutant EML4-ALK, AP26113 was active at IC50s of 10 and 24 nM, respectively. [3]
Targets
Target Value
Product Information
Catalog Num A11948
Formula C26H34ClN6O2P
Molecular Weight 529.01
CAS Number 1197958-12-5
SMILES CN(C)C1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=CC=C4P(=O)(C)C)Cl)OC
Synonyms AP-26113
Storage

Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for 36 months.
In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Solubility
In vitro (25°C) DMSO 40 mg/mL (75.61 mM)
Water Insoluble
Ethanol 93 mg/mL (175.8 mM)
In vivo NMP+PEG300 (10+90, v+v) 28 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Preparing Stock Solutions
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 18.9 mL 94.52 mL 189.03 mL
0.5 mM 3.78 mL 18.9 mL 37.81 mL
1 mM 1.89 mL 9.45 mL 18.9 mL
5 mM 0.38 mL 1.89 mL 3.78 mL
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